Calcium channel blocker indications

ACE inhibitors can be administered with diuretics (qv), cardiac glycosides, -adrenoceptor blockers, and calcium channel blockers. Clinical trials indicate they are generally free from serious side effects. The effectiveness of enalapril, another ACE inhibitor, in preventing patient mortaUty in severe (Class IV) heart failure was investigated. In combination with conventional dmgs such as vasodilators and diuretics, a 40% reduction in mortaUty was observed after six months of treatment using 2.5—40 mg/d of enalapril (141). However, patients complain of cough, and occasionally rash and taste disturbances can occur. 

Procardia XL. Procardia XL extended-release capsules, marketed by Pfizer Labs Division of Pfizer, Inc., contain nifedipine [21829-25-4] a calcium channel blocker of mol wt 346.3. The extended release tablet is formulated as a once-a-day controlled release capsule for oral adrninistration dehvering either 30, 60, or 90 mg nifedipine. Procardia XL is indicated for use in the management of vasospastic angina, chronic stable angina, and hypertension (see Cardiovascularagents). 

Amlodipine and nifedipine are dihydropyridine calcium-channel blockers. Amlodipine differs from nifedipine in that it has a longer duration of action and can therefore be given once daily, unlike nifedipine. Both are indicated in hypertension and angina and tend to cause ankle oedema that does not respond to diuretic therapy. Neither amlodipine nor nifedipine are available as spray formulations. 

Calcium channel blockers are not indicated for routine use in this stage. 

There has been some concern about the safety of the calcium channel blockers. In particular, reports indicated that certain calcium channel blockers, such as the short-acting form of nifedipine, may be associated with an increased risk of myocardial infarction in certain patients (older patients with hypertension, patients with unstable angina).21,29... 

Activation of platelets is considered an essential process for arterial thrombosis. Thus, treatment with platelet-inhibiting drugs such as aspirin and ticlopidine or clopidogrel is indicated in patients with transient ischemic attacks and strokes or unstable angina and acute myocardial infarction. In angina and infarction, these drugs are often used in conjunction with -blockers, calcium channel blockers, and fibrinolytic drugs. 

Verapamil and diltiazem are prototypic calcium channel blockers. As indicated previously, these drugs influence cardiac function by blocking inward calcium movement through L channels. In so doing they block conduction velocity in SA and AV node cells. They are used therapeutically to treat reentry arrhythmias through the AV node as well as paroxysmal supraventricular tachycardias. In fact, verapamil has been reported to terminate 60-80 percent of paroxysmal supraventricular tachycardias within several minutes. However, because of their potent effect on AV conduction, these drugs are contraindicated in patients with preexisting conduction problems since they may produce complete AV block. 

The calcium channel blockers are divided into three chemical classes, each with different pharmacokinetic properties and clinical indications (Figures 19.11 and 19.12). 

Examples of such calcium channel blockers are shown in Figure 6.7. While nifedipine contains the dihydropyridine moiety (in red) after which the receptor has been named, verapamil does not, indicating that the receptor s name does not reflect any fundamental requirement of drug molecular structure. 

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